Details

Autor(en) / Beteiligte

• Blaquiere, Nicole
• Villemure, Elisia
• Staben, Steven T

Titel

Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases

Ist Teil von

• Journal of medicinal chemistry, 2020-08, Vol.63 (15), p.7957-7985

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

2020

Link zum Volltext

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• The ubiquitin proteasome system (UPS) presents many opportunities for pharmacological intervention. Key players in the UPS are E3 ubiquitin ligases, responsible for conjugation of ubiquitin to specific cognate substrates. Numbering more than 600 members, these ligases represent the most selective way to intervene within this physiologically important system. This Perspective highlights some of the dedicated medicinal chemistry efforts directed at inhibiting the function of specific single-protein and multicomponent RING-type E3 ubiquitin ligases. We present opportunities and challenges associated with targeting this important class of enzymes.